JP2020518581A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020518581A5 JP2020518581A5 JP2019559297A JP2019559297A JP2020518581A5 JP 2020518581 A5 JP2020518581 A5 JP 2020518581A5 JP 2019559297 A JP2019559297 A JP 2019559297A JP 2019559297 A JP2019559297 A JP 2019559297A JP 2020518581 A5 JP2020518581 A5 JP 2020518581A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- compound
- disease
- form according
- crystal form
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 42
- 239000013078 crystal Substances 0.000 claims description 33
- 239000000203 mixture Substances 0.000 claims description 25
- 241000124008 Mammalia Species 0.000 claims description 22
- 230000004064 dysfunction Effects 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 21
- 230000000735 allogeneic effect Effects 0.000 claims description 18
- 208000030533 eye disease Diseases 0.000 claims description 17
- 208000023504 respiratory system disease Diseases 0.000 claims description 17
- 230000001684 chronic effect Effects 0.000 claims description 16
- 210000004072 lung Anatomy 0.000 claims description 16
- 239000002904 solvent Substances 0.000 claims description 16
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 14
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 12
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 12
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 12
- 206010051604 Lung transplant rejection Diseases 0.000 claims description 12
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 12
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 12
- 208000027866 inflammatory disease Diseases 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 10
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims description 10
- 208000006673 asthma Diseases 0.000 claims description 10
- 201000011190 diabetic macular edema Diseases 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims description 8
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims description 8
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 8
- 206010046851 Uveitis Diseases 0.000 claims description 8
- 238000010438 heat treatment Methods 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 8
- 206010006451 bronchitis Diseases 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 7
- 239000003937 drug carrier Substances 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 7
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 6
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 6
- 206010012438 Dermatitis atopic Diseases 0.000 claims description 6
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 6
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 6
- 206010014561 Emphysema Diseases 0.000 claims description 6
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 6
- 206010067472 Organising pneumonia Diseases 0.000 claims description 6
- 206010035664 Pneumonia Diseases 0.000 claims description 6
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims description 6
- 230000001154 acute effect Effects 0.000 claims description 6
- 206010069351 acute lung injury Diseases 0.000 claims description 6
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims description 6
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 6
- 201000008937 atopic dermatitis Diseases 0.000 claims description 6
- 206010069664 atopic keratoconjunctivitis Diseases 0.000 claims description 6
- 201000009805 cryptogenic organizing pneumonia Diseases 0.000 claims description 6
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 6
- 230000000527 lymphocytic effect Effects 0.000 claims description 6
- 208000002780 macular degeneration Diseases 0.000 claims description 6
- 210000000440 neutrophil Anatomy 0.000 claims description 6
- 208000004644 retinal vein occlusion Diseases 0.000 claims description 6
- 238000002054 transplantation Methods 0.000 claims description 6
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 4
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims description 4
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 4
- 239000008240 homogeneous mixture Substances 0.000 claims description 4
- LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 claims description 4
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 4
- 230000001568 sexual effect Effects 0.000 claims description 4
- 239000002002 slurry Substances 0.000 claims description 4
- -1 2- (6- (2-ethyl-5-fluoro-4-hydroxyphenyl) -4-fluoro-1H-indazole-3-yl) -1,4,6,7-tetrahydro-5H -Imidazo [4,5-c] Pyridine-5-yl Chemical group 0.000 claims description 2
- 206010012692 Diabetic uveitis Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 239000000375 suspending agent Substances 0.000 claims description 2
- XPDSWOKOBJJMMX-UHFFFAOYSA-N CCc(cc(c(F)c1)O)c1-c1cc([nH]nc2-c3nc(CN(CC4)C(CN5CCOCC5)=O)c4[n]3C)c2c(F)c1 Chemical compound CCc(cc(c(F)c1)O)c1-c1cc([nH]nc2-c3nc(CN(CC4)C(CN5CCOCC5)=O)c4[n]3C)c2c(F)c1 XPDSWOKOBJJMMX-UHFFFAOYSA-N 0.000 description 1
- 229940125904 compound 1 Drugs 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000013160 medical therapy Methods 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762492574P | 2017-05-01 | 2017-05-01 | |
| US62/492,574 | 2017-05-01 | ||
| PCT/US2018/030148 WO2018204238A1 (en) | 2017-05-01 | 2018-04-30 | Fused imidazo-piperidine jak inhibitor compound |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020518581A JP2020518581A (ja) | 2020-06-25 |
| JP2020518581A5 true JP2020518581A5 (enExample) | 2021-05-06 |
| JP7098656B2 JP7098656B2 (ja) | 2022-07-11 |
Family
ID=62165730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019559297A Active JP7098656B2 (ja) | 2017-05-01 | 2018-04-30 | 縮合イミダゾピペリジンｊａｋ阻害剤化合物 |
Country Status (32)
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20180073687A (ko) | 2015-11-03 | 2018-07-02 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 호흡기 질환의 치료를 위한 jak 키나제 저해제 화합물 |
| AU2018231035B2 (en) | 2017-03-09 | 2021-09-09 | Theravance Biopharma R&D Ip, Llc | Fused imidazo-piperidine JAK inhibitors |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
| EP3609498A1 (en) | 2017-05-01 | 2020-02-19 | Theravance Biopharma R&D IP, LLC | Methods of treatment using a jak inhibitor compound |
| AU2019335199A1 (en) | 2018-09-04 | 2021-03-11 | Theravance Biopharma R&D Ip, Llc | Process for preparing jak inhibitors and intermediates thereof |
| US10836763B2 (en) | 2018-09-04 | 2020-11-17 | Theravance Biopharma R&D Ip, Llc | 5 to 7 membered heterocyclic amides as JAK inhibitors |
| JP7324836B2 (ja) | 2018-09-04 | 2023-08-10 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋ阻害剤としてのジメチルアミノアゼチジンアミド |
| KR20210084512A (ko) | 2018-10-29 | 2021-07-07 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | Jak 억제제로서 2-아자비시클로 헥산 화합물 |
| JP7680955B2 (ja) | 2019-01-11 | 2025-05-21 | ネイジス ファーマシューティカルズ インコーポレイテッド | ロイコトリエン合成阻害剤 |
| HUE067145T2 (hu) * | 2019-02-25 | 2024-10-28 | Henan Medinno Pharmaceutical Tech Co Ltd | JAK inhibitor vegyület és alkalmazása |
| MA55201A (fr) | 2019-03-05 | 2022-01-12 | Incyte Corp | Inhibiteurs de la voie jak1 pour le traitement d'un dysfonctionnement chronique de l'allogreffe pulmonaire |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| TW202144343A (zh) | 2020-03-02 | 2021-12-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Jak抑制劑化合物之結晶水合物 |
| CN115244047A (zh) * | 2020-03-18 | 2022-10-25 | 四川海思科制药有限公司 | 一种吲唑衍生物及其在医药上的应用 |
| CN111620868B (zh) * | 2020-05-28 | 2021-08-31 | 爱斯特（成都）生物制药股份有限公司 | 一种1H-吡唑并[3,4-b]吡啶-3-甲醛的制备方法 |
| JP2024524214A (ja) * | 2021-06-25 | 2024-07-05 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋ阻害剤としてのイミダゾロインダゾール化合物 |
| CN114181055A (zh) * | 2021-12-21 | 2022-03-15 | 苏州楚凯药业有限公司 | 1-苄氧基-4-溴-5-乙基-2-氟苯的制备方法 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI262914B (en) | 1999-07-02 | 2006-10-01 | Agouron Pharma | Compounds and pharmaceutical compositions for inhibiting protein kinases |
| US7872014B2 (en) | 2003-07-23 | 2011-01-18 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| US20050090529A1 (en) | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| US7884109B2 (en) | 2005-04-05 | 2011-02-08 | Wyeth Llc | Purine and imidazopyridine derivatives for immunosuppression |
| US8648069B2 (en) | 2007-06-08 | 2014-02-11 | Abbvie Inc. | 5-substituted indazoles as kinase inhibitors |
| JP2010111624A (ja) | 2008-11-06 | 2010-05-20 | Shionogi & Co Ltd | Ｔｔｋ阻害作用を有するインダゾール誘導体 |
| US20120029190A1 (en) | 2009-04-03 | 2012-02-02 | Douglas Burdi | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| SMT201700581T1 (it) | 2009-12-21 | 2018-01-11 | Samumed Llc | 1h-pirazolo[3,4-b]piridine e loro usi terapeutici |
| US8575336B2 (en) | 2011-07-27 | 2013-11-05 | Pfizer Limited | Indazoles |
| NZ720092A (en) | 2013-12-05 | 2019-05-31 | Pfizer | Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides |
| CA2948587C (en) | 2014-05-14 | 2018-07-17 | Pfizer Inc. | Pyrazolopyridines and pyrazolopyrimidines |
| WO2016026078A1 (en) | 2014-08-19 | 2016-02-25 | Changzhou Jiekai Pharmatech Co., Ltd. | Heterocyclic compounds as erk inhibitors |
| KR101663277B1 (ko) | 2015-03-30 | 2016-10-06 | 주식회사 녹십자 | TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물 |
| EP3371185B1 (en) | 2015-11-03 | 2020-09-30 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors |
| EP3712152B1 (en) | 2015-11-03 | 2021-01-13 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors |
| KR20180073687A (ko) | 2015-11-03 | 2018-07-02 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 호흡기 질환의 치료를 위한 jak 키나제 저해제 화합물 |
| AU2018231035B2 (en) | 2017-03-09 | 2021-09-09 | Theravance Biopharma R&D Ip, Llc | Fused imidazo-piperidine JAK inhibitors |
| JP7096268B2 (ja) | 2017-05-01 | 2022-07-05 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋ阻害剤化合物の結晶形態 |
| EP3609498A1 (en) | 2017-05-01 | 2020-02-19 | Theravance Biopharma R&D IP, LLC | Methods of treatment using a jak inhibitor compound |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
-
2018
- 2018-04-27 AR ARP180101103A patent/AR111495A1/es unknown
- 2018-04-30 WO PCT/US2018/030148 patent/WO2018204238A1/en not_active Ceased
- 2018-04-30 MX MX2019012942A patent/MX388751B/es unknown
- 2018-04-30 US US15/966,467 patent/US10493077B2/en active Active
- 2018-04-30 JP JP2019559297A patent/JP7098656B2/ja active Active
- 2018-04-30 HR HRP20220330TT patent/HRP20220330T1/hr unknown
- 2018-04-30 BR BR112019022648A patent/BR112019022648A2/pt not_active IP Right Cessation
- 2018-04-30 PL PL18724754T patent/PL3601283T3/pl unknown
- 2018-04-30 SI SI201830589T patent/SI3601283T1/sl unknown
- 2018-04-30 LT LTEPPCT/US2018/030148T patent/LT3601283T/lt unknown
- 2018-04-30 ES ES18724754T patent/ES2908756T3/es active Active
- 2018-04-30 KR KR1020197035134A patent/KR102550225B1/ko active Active
- 2018-04-30 EP EP18724754.9A patent/EP3601283B1/en active Active
- 2018-04-30 MA MA47970A patent/MA47970B1/fr unknown
- 2018-04-30 UA UAA201911546A patent/UA124478C2/uk unknown
- 2018-04-30 NZ NZ757570A patent/NZ757570A/en not_active IP Right Cessation
- 2018-04-30 SG SG11201908604Y patent/SG11201908604YA/en unknown
- 2018-04-30 DK DK18724754.9T patent/DK3601283T3/da active
- 2018-04-30 AU AU2018261593A patent/AU2018261593B2/en not_active Ceased
- 2018-04-30 RS RS20220238A patent/RS62995B1/sr unknown
- 2018-04-30 PT PT187247549T patent/PT3601283T/pt unknown
- 2018-04-30 MD MDE20200142T patent/MD3601283T2/ro not_active IP Right Cessation
- 2018-04-30 TW TW107114647A patent/TWI760486B/zh not_active IP Right Cessation
- 2018-04-30 EA EA201992601A patent/EA201992601A1/ru unknown
- 2018-04-30 CA CA3056283A patent/CA3056283A1/en active Pending
- 2018-04-30 CN CN201880028413.7A patent/CN110573508B/zh not_active Expired - Fee Related
- 2018-04-30 SM SM20220079T patent/SMT202200079T1/it unknown
-
2019
- 2019-09-30 PH PH12019502264A patent/PH12019502264A1/en unknown
- 2019-10-18 US US16/656,940 patent/US11160810B2/en not_active Expired - Fee Related
- 2019-10-24 CO CONC2019/0011809A patent/CO2019011809A2/es unknown
- 2019-10-28 IL IL270231A patent/IL270231B2/en unknown
- 2019-10-28 CL CL2019003086A patent/CL2019003086A1/es unknown
-
2021
- 2021-09-28 US US17/449,131 patent/US20220008428A1/en not_active Abandoned
-
2022
- 2022-03-09 CY CY20221100192T patent/CY1125051T1/el unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020518581A5 (enExample) | ||
| HRP20220330T1 (hr) | Kondenzirani imidazopiperidinski spoj, kao inhibitor jak | |
| JP2019517463A5 (enExample) | ||
| RU2020121150A (ru) | Твердые формы ингибитора калликреина плазмы и его солей | |
| US8809367B2 (en) | 1-1-Oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives as N-formyl peptide receptor like-1 (FPRL-1) receptor modulators | |
| CA3025720A1 (en) | Polymorphs of n-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1 -({4-[2-oxopyridin-1 -yl)methyl]phenyl} methyl) pyrazole -4-carboxamide as kallikrein inhibitors | |
| JP2021504310A5 (enExample) | ||
| JP2018531982A5 (enExample) | ||
| JP2020518582A5 (enExample) | ||
| JP2018531963A (ja) | バルベナジン塩およびその多形体 | |
| WO2019141179A1 (zh) | 吡啶酮衍生物、其组合物及作为抗流感病毒药物的应用 | |
| CN109071491B (zh) | 吲唑的合成 | |
| JP2019509268A5 (enExample) | ||
| WO2003087086A2 (de) | Substituierte indole und deren verwendung als 5ht-wiederaufnahme inhibitoren und als 5ht liganden | |
| JP2021501151A5 (enExample) | ||
| JP2017512786A5 (enExample) | ||
| KR20150036767A (ko) | A2a 효능제로서의 n-알킬 2-(이치환된)알키닐아데노신-5-유론아미드 | |
| CN110776481B (zh) | 一类双阳离子化合物及其制备方法和用途 | |
| JP2004307440A (ja) | ２−アミノ‐１，３‐プロパンジオール誘導体とその付加塩 | |
| KR20120098816A (ko) | 메틸｛４，６?디아미노?２?〔１?（２?플루오로벤질）?１ｈ?피라졸로〔３，４?ｂ〕피리딘?３?일〕피리미딘?５?일｝카르바메이트의 신규한 다형체 형상 | |
| CN102471273B (zh) | 2-[[[2-[(羟基乙酰基)氨基]-4-吡啶基]甲基]硫代]-n-[4-(三氟甲氧基)苯基]-3-吡啶甲酰胺苯磺酸盐、其晶体、其多晶型物以及用于制备其的方法 | |
| JPWO2019220390A5 (enExample) | ||
| CN101914056B (zh) | 一种n-烷基取代四氢咔唑酮衍生物的制备方法 | |
| WO2015011659A1 (en) | Crystalline polymorphic forms of regorafenib and processes for the preparation of polymorph i of regorafenib | |
| AU2001246577B2 (en) | Pyridazinyl phenyl hydrazones useful against congestive heart failure |